The invention is related to phenanthrofuran derivatives whose properties include anti-angiogenic activity.
Angiogenesis, or neovascularization, is the process of the growth of capillary blood vessels. The disturbances in the regulation of angiogenesis are associated with angiogenic diseases such as arthritis, psoriasis, diabetic retinopathy, hemangiomas, and cancer including tumor growth and metastasis. Endogenous angiogenic factors include basic fibroblast growth factor (b-FGF), vascular permeability factor/vascular endothelial growth factor, angiogenin, granulocyte-colony stimulating factor (G-CSF), heparinases, interleukin 8 (IL-8), platelet derived growth factor (PD-GF), placenta growth factor, prostaglandin E1 (PGE1), prostaglandin E2 (PGE2), hepatocyte growth factor, TGF-.alpha., TGF-.beta., TNF-.alpha., and TNF-.beta.. Anti-angiogenic factors include angiostatin, cartilage-derived inhibitor, interferon-.alpha. (IFN-.alpha.), interferon-.beta. (IFN-.beta.), protamine, thrombspondin, and tissue inhibitors of metalloproteinase (TIMPs).
Ajuforrestine A was isolated from the whole plant of Ajuga forrestii Diels (Wang et al., Chinese Chem. Lett. 5:125, 1994). According to Wang et al., the whole plant is used as a traditional herbal medicine for the treatment of dysentery, laryngitis, and acute and chronic nephritis (brightism).